| UNBS1450, a steroid cardiac glycoside inducing apoptotic cell death in human leukemia cells. | |
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MedLine Citation:
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PMID: 20849830 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Cardiac steroids are used to treat various diseases including congestive heart failure and cancer. The aim of this study was to investigate the anti-leukemic activity of UNBS1450, a hemi-synthetic cardenolide belonging to the cardiac steroid glycoside family. Here, we report that, at low nanomolar concentrations, UNBS1450 induces apoptotic cell death. Subsequently, we have investigated the molecular mechanisms leading to apoptosis activation. Our results show that UNBS1450 inhibits NF-κB transactivation and triggers apoptosis by cleavage of pro-caspases 8, 9 and 3/7, by decreasing expression of anti-apoptotic Mcl-1 and by recruitment of pro-apoptotic Bak and Bax protein eventually resulting in cell death. |
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Authors:
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Tom Juncker; Claudia Cerella; Marie-Hélène Teiten; Franck Morceau; Marc Schumacher; Jenny Ghelfi; François Gaascht; Michael Schnekenburger; Estelle Henry; Mario Dicato; Marc Diederich |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-09-21 |
Journal Detail:
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Title: Biochemical pharmacology Volume: 81 ISSN: 1873-2968 ISO Abbreviation: Biochem. Pharmacol. Publication Date: 2011 Jan |
Date Detail:
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Created Date: 2010-11-24 Completed Date: 2010-12-30 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0101032 Medline TA: Biochem Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 13-23 Citation Subset: IM |
Copyright Information:
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Copyright © 2010 Elsevier Inc. All rights reserved. |
Affiliation:
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Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Fondation de Recherche Cancer et Sang, Hôpital Kirchberg, 9 Rue Edward Steichen, 2540 Luxembourg, Luxembourg. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Apoptosis
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drug effects* Cardenolides / chemistry, pharmacology* Cell Line Gene Expression Regulation, Neoplastic Humans Leukemia / drug therapy* Molecular Structure Neoplasm Proteins / genetics, metabolism |
| Chemical | |
Reg. No./Substance:
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0/Cardenolides; 0/Neoplasm Proteins; 0/UNBS 1450 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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